Elagolix-d6 (natrium)

Elagolix-d6 (sodium) (NBI-56418-d6 (sodium) ) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. [1][2][3][4][5].

NBI-56418-d6 (sodium)

12352005

GnRH Receptor; Isotope-Labeled Compounds; Nuclear Factor of activated T Cells (NFAT)

GPCR/G Protein; Immunology/Inflammation; Others

Metabolism-protein/nucleotide metabolism

Endocrinology; Cancer

O=C(O[Na])C([2H])([2H])C([2H])([2H])C([2H])([2H])N[C@H](C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3C4=CC=CC(OC)=C4F)=O)C3=O

C32H23D6F5N3NaO5

659.61

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Kim SM, et al. Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. J Med Chem. 2016 Oct 13;59 (19) :9150-9172. Epub 2016 Sep 27.|[3]Chen C, et al. Discovery of sodium R- (+) -4-{2-[5- (2-fluoro-3-methoxyphenyl) -3- (2-fluoro-6-[trifluoromethyl]benzyl) -4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11;51 (23) :7478-85.|[4]Qiong Wang, et al. Analytical methodology and pharmacokinetic study of elagolix in plasma of rats using a newly developed UPLC-MS/MS assay. Arabian Journal of Chemistry. Volume 14, Issue 7, July 2021, 103235|[5]Mohammad Ezzati, et al. Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain. Womens Health (Lond) . 2015 Jan;11 (1) :19-28.|[6]Carr B, et al. Elagolix, an oral GnRH antagonist, versus subcutaneous depot medroxyprogesterone acetate for the treatment of endometriosis: effects on bone mineral density. Reprod Sci. 2014 Nov;21 (11) :1341-1351.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-W751574/

Isotope-Labeled Compounds

No Development Reported